The present invention relates to novel compounds useful as gastrointestinal function promoting agents. More particularly, the present invention relates to the application of novel derivatives of erythromycin to gastrointestinal function promoting agents.
The antibiotic erythromycin, which belongs to the class of basic 14-membered ring macrolides, is produced from microorganisms such as the strains described in J. M. McGuire et al., Antibiotics & Chemotherapy, 2, 281-283 (1952) and D. P. Labeda et al., Int. J. Syst. Bacteriol., 37, 19-22 (1987) and represented by Streptomyces erythreus (Saccharopolyspora erythraea), and is composed of erythromycins A, B, C and D as shown below [P. F. Wiley et al., J. Amer. Chem. Soc., 79, 6062-6070, 6070-6073, 6074-6077 (1957); J. Majer et al., J. Amer. Chem. Soc., 99, 1620-1622 (1977)].
______________________________________ ##STR1## ERM X.sub.1 X.sub.2 ______________________________________ A OH CH.sub.3 B H CH.sub.3 C OH H D H H ______________________________________
Erythromycin (hereinafter sometimes abbreviated as ERM) A in its use as an antibacterial agent can have side effects such as vomiting. Z. Itoh et al. has reported that ERM A has motilin-like action promoting the gastrointestinal peristaltic movement [gastrointestinal motor stimulating (hereinafter occasionally reffered to as GMS) activity] [Am. J. Physiol., 247, G688-694 (1984)]. S. Omura et al. reported preparing ERM derivatives having a strong GMS activity in which little antibacterial effect was observed, and filed applications for patents (EP-A-213617 and EP-A-215355). Manufacturing methods, properties, structures and biological activity of these derivatives are described in J. Med. Chem., 30, 1941-1943 (1987) and Chem. Pharm. Bull., 37, 2687-2700, 2701-2709 (1989).
Humans eat food to support life and to maintain and restore physical strength. However, an individual's whose digestive function or whose gastrointestinal motor function is lowered, such as a patient after an operation, a patient with a grave infectious disease or cancer, a patient with diabetes in whom a gastrointestinal functional disorder is observed, a patient with chronic gastritis or a patient with regurgitant esophagitis, requires a drug to activate the gastrointestinal motor function. Accordingly, the development of an excellent gastrointestinal motor promoting agent is needed.